Irreversible Inhibition of DNMT3A by an N-Mustard Analog of S-Adenosyl-L-methionine
Nichanun Sirasunthorn,
Isabelle Roseto,
Lindsay Pecor
et al.
Abstract:DNA methylation, an important epigenetic modification, is catalyzed by DNA methyltransferases and is essential in the regulation of gene expression. Here, the utility of an N-mustard analog designed to mimic the native methyl donor, S-adenosyl-L-methionine (SAM), was explored with the DNA methyltransferase 3A catalytic domain (DNMT3AC). In lieu of the expected analog transfer to DNA, methyltransferase activity was instead inhibited in a concentration dependent manner. Further investigation into the mechanism o… Show more
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